The Pharmacokinetics of Enhancement of Cyclosporin A by Berberine Chloride Coadministrated in Renal Transplanted Recipients

OBJECTIVE: To study the pharmacokinetics of cyclosporin A (CsA) with or without combination of berberine chloride(Ber)in renal transplanted recipients. METHODS:This study included 6 patients treated with cyclosporin A at 6 mg.g-1d-1 for two weeks within one month of renal transplantation. Each patient was involved in pharmacokinetics of cyclosporin A before and after coadministration of berberine hydrochride by fluorescence polarization immunoassay. RESULTS: The pharmacokinetic parameters of cyclosporin A before coadministration of berberine were:t(1/2):2.62±1.OOh,tmax:1.33±0.52h,Cmax:1224.75±296.20μg.L-1, Cmin:173.95 ±78.71μg.L-1,AUC: 4681.34±1300.45μg.h.L-1,CL/F: 35±15L.h-1.The pharmacokinetic parameters of cyclosporin A after coadministration of berberine hydro chloride were: t(1/2): 5.33±2.6,AUC:6265.71±1871.33μg.h.L-1,CL/F:22± 13L.h-1. CONCLUSION: berberine hydro chloride could markedly elevate the blood concentration of cyclosporin A in renal transplanted recipients. After coadministration of berberine hydro chloride, tmax of cyclosporin A was delayed and CL was decreased while t1/2, and A UC were increased. Two drug coadministration had no effects on liver and renal function.